ChEMBL ligand: CHEMBL28324 (KN-62)
calcium/calmodulin-dependent protein kinase II alpha subunit/CaM kinase II alpha in Human [ChEMBL: CHEMBL4147] [GtoPdb: 1555] [UniProtKB: Q9UQM7] There should be some charts here, you may need to enable JavaScript!
calcium/calmodulin-dependent protein kinase II delta subunit/CaM kinase II delta in Human [ChEMBL: CHEMBL2801] [GtoPdb: 1558] [UniProtKB: Q13557] There should be some charts here, you may need to enable JavaScript!
P2X7 purinoceptor in Dog [ChEMBL: CHEMBL3600277] [UniProtKB: Q64F92] There should be some charts here, you may need to enable JavaScript!
P2X purinoceptor in Guinea pig [ChEMBL: CHEMBL3600276] [UniProtKB: A9QW74] There should be some charts here, you may need to enable JavaScript!
P2X4/P2X purinoceptor 4 in Human [ChEMBL: CHEMBL2104] [GtoPdb: 481] [UniProtKB: Q99571] There should be some charts here, you may need to enable JavaScript!
P2X7/P2X purinoceptor 7 in Human [ChEMBL: CHEMBL4805] [GtoPdb: 484] [UniProtKB: Q99572] P2X7/P2X purinoceptor 7 in Rat [ChEMBL: CHEMBL2496] [GtoPdb: 484] [UniProtKB: Q64663] There should be some charts here, you may need to enable JavaScript!
Calmodulin-dependent kinase II in Human [GtoPdb: 1554] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
calcium/calmodulin-dependent protein kinase II alpha subunit/CaM kinase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4147] [GtoPdb: 1555] [UniProtKB: Q9UQM7]
ChEMBL	Inhibition of human CaMKIIalpha using calmodulin and syntide-2 incubated for 15 mins by ELISA	B	5.99	pIC50	1030	nM	IC50	J Med Chem (2020) 63: 1313-1327 [PMID:31972088]
calcium/calmodulin-dependent protein kinase II delta subunit/CaM kinase II delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2801] [GtoPdb: 1558] [UniProtKB: Q13557]
ChEMBL	Inhibition of human recombinant CAMK2delta using tetramethylbenzidine as substrate by spectrophotometry analysis	B	6.42	pIC50	380	nM	IC50	Bioorg Med Chem (2012) 20: 377-400 [PMID:22112539]
P2X7 purinoceptor in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3600277] [UniProtKB: Q64F92]
ChEMBL	Inhibition of dog P2X7 receptor	B	8	pIC50	10	nM	IC50	Bioorg Med Chem Lett (2015) 25: 3164-3167 [PMID:26099538]
P2X purinoceptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3600276] [UniProtKB: A9QW74]
ChEMBL	Inhibition of guinea pig P2X7 receptor	B	6.89	pIC50	130	nM	IC50	Bioorg Med Chem Lett (2015) 25: 3164-3167 [PMID:26099538]
P2X4/P2X purinoceptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2104] [GtoPdb: 481] [UniProtKB: Q99571]
ChEMBL	Antagonist activity against recombinant human P2X purinoceptor 4 (P2X4)	F	4	pEC50	100000	nM	EC50	J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
P2X7/P2X purinoceptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4805] [GtoPdb: 484] [UniProtKB: Q99572]
ChEMBL	Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium bromide uptake after 2 hrs by fluorescence assay	B	4.02	pIC50	96000	nM	IC50	Bioorg Med Chem Lett (2017) 27: 759-763 [PMID:28126517]
ChEMBL	Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced fluorescent ethidium accumulation	F	6.47	pIC50	340	nM	IC50	Bioorg Med Chem Lett (2009) 19: 954-958 [PMID:19110420]
ChEMBL	Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced pore formation	F	6.52	pIC50	300	nM	IC50	Bioorg Med Chem (2009) 17: 4861-4865 [PMID:19540765]
ChEMBL	Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium bromide uptake after 2 hrs by fluorescence analysis	F	6.55	pIC50	280	nM	IC50	J Med Chem (2012) 55: 3687-3698 [PMID:22400713]
ChEMBL	Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium ion uptake after 2 hrs	B	6.6	pIC50	250	nM	IC50	Eur J Med Chem (2015) 106: 180-193 [PMID:26547056]
ChEMBL	Antagonist activity at recombinant human P2X7 receptor assessed as inhibition of BzATP-mediated Yo-Pro uptake measured for 1 hr by FLIPR assay	B	6.68	pIC50	210	nM	IC50	Eur J Med Chem (2013) 70: 811-830 [PMID:24246730]
ChEMBL	Antagonist activity at human purinergic P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium bromide uptake	F	6.76	pIC50	175	nM	IC50	Bioorg Med Chem Lett (2008) 18: 571-575 [PMID:18078749]
ChEMBL	Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake after 2 hrs by fluorescence assay relative to control	B	6.8	pIC50	158	nM	IC50	Eur J Med Chem (2018) 151: 462-481 [PMID:29649742]
ChEMBL	Antagonist activity at human P2X7 receptor in expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake	B	6.8	pIC50	158	nM	IC50	Eur J Med Chem (2018) 151: 462-481 [PMID:29649742]
ChEMBL	Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced accumulation of ethidium+ after 120 mins by fluorescence assay	B	6.8	pIC50	158	nM	IC50	Eur J Med Chem (2013) 70: 811-830 [PMID:24246730]
ChEMBL	Antagonist activity at P2X7 receptor in human lymphocytes assessed as inhibition of ATP-induced ethidium ion uptake preincubated for 5 mins followed by ATP addition and incubated further 2 mins prior to ethidium addition measured up to 5 mins by flow cytometric analysis	B	6.8	pIC50	158	nM	IC50	Eur J Med Chem (2015) 106: 180-193 [PMID:26547056]
ChEMBL	Antagonist activity at recombinant human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced intracellular ethidium bromide uptake after 2 hrs by fluorescence assay	B	6.8	pIC50	158	nM	IC50	J Med Chem (2015) 58: 2114-2134 [PMID:25597334]
ChEMBL	Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release preincubated for 30 mins followed by BzATP induction measured after 30 mins by ELISA	B	6.84	pIC50	143	nM	IC50	J Med Chem (2015) 58: 2114-2134 [PMID:25597334]
ChEMBL	Antagonist activity at P2X7 in LPS/IFN gamma differentiated human THP-1 cells assessed as inhibition of BzATP-induced IL-1beta release preincubated for 30 mins followed by BzATP stimulation for 30 mins by ELISA	B	6.89	pIC50	130	nM	IC50	Eur J Med Chem (2018) 151: 462-481 [PMID:29649742]
ChEMBL	Antagonist activity at P2X7 receptor expressed in LPS/IFNgamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta production after 4 hrs by ELISA	B	6.89	pIC50	129	nM	IC50	Eur J Med Chem (2015) 106: 180-193 [PMID:26547056]
ChEMBL	Antagonist activity at human P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced IL8 release pretreated for 30 mins before bzATP challenge measured after 30 mins by ELISA	F	6.92	pIC50	120	nM	IC50	J Med Chem (2012) 55: 3687-3698 [PMID:22400713]
ChEMBL	Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced fluorescent ethidium accumulation at 10 uM	F	6.96	pIC50	110	nM	IC50	Bioorg Med Chem Lett (2009) 19: 6053-6058 [PMID:19800793]
ChEMBL	Inhibition of human P2X7 receptor	B	7	pIC50	100	nM	IC50	Bioorg Med Chem Lett (2015) 25: 3164-3167 [PMID:26099538]
ChEMBL	Antagonist activity at P2X7 receptor (unknown origin)	B	7.03	pIC50	94.4	nM	IC50	Bioorg Med Chem (2014) 22: 54-88 [PMID:24314880]
ChEMBL	Antagonistic activity against P2X7 receptor measured as the ATP dependent calcium influx in human monocytes	F	7.29	pIC50	51.1	nM	IC50	J Med Chem (2003) 46: 1318-1329 [PMID:12672232]
ChEMBL	Antagonist activity at human P2X7 receptor	B	7.29	pIC50	51	nM	IC50	J Med Chem (2015) 58: 2114-2134 [PMID:25597334]
ChEMBL	Antagonistic activity against P2X7 receptor	F	7.29	pIC50	51	nM	IC50	Bioorg Med Chem Lett (2003) 13: 4047-4050 [PMID:14592505]
ChEMBL	Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium influx	F	7.3	pIC50	50.12	nM	IC50	J Med Chem (2009) 52: 3123-3141 [PMID:19191585]
ChEMBL	Inhibitory concentration was evaluated against P2X purinoceptor 7	B	7.87	pIC50	13.4	nM	IC50	Bioorg Med Chem Lett (2000) 10: 681-684 [PMID:10762053]
ChEMBL	Antagonist activity at P2X7 receptor in human lymphocytes assessed as inhibition of ATP-induced Ba2+ influx	F	7.9	pIC50	12.59	nM	IC50	J Med Chem (2009) 52: 3123-3141 [PMID:19191585]
ChEMBL	Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release preincubated for 30 mins followed by BzATP induction measured after 30 mins by ELISA	B	7.9	pIC50	12.59	nM	IC50	J Med Chem (2015) 58: 2114-2134 [PMID:25597334]
ChEMBL	Antagonist activity against recombinant human P2X purinoceptor 7 (P2X7)	F	7.47	pEC50	34	nM	EC50	J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
P2X7/P2X purinoceptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2496] [GtoPdb: 484] [UniProtKB: Q64663]
ChEMBL	Inhibition of rat P2X7 receptor	B	4	pIC50	>100000	nM	IC50	Bioorg Med Chem Lett (2015) 25: 3164-3167 [PMID:26099538]
Calmodulin-dependent kinase II in Human [GtoPdb: 1554]
GtoPdb	-	-	6.05	pIC50	900	nM	IC50	J Biol Chem (1990) 265: 4315-20 [PMID:2155222]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]